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Endocrinology-Hormones

Small molecules play a pivotal role in Endocrinology Research. These are low molecular weight compounds that have a significant impact on the endocrine system, hormones, and their receptors. Here are some key aspects of how small molecules are involved in this field:

  • Hormone Mimetics and Inhibitors: Small molecules are used to develop synthetic compounds that mimic the actions of hormones or inhibit their effects. For example, drugs like metformin for diabetes management and selective estrogen receptor modulators (SERMs) for breast cancer treatment are used to either mimic or block hormonal activity.
  • Receptor Modulation: Small molecules can bind to hormone receptors and modulate their activity. This is crucial in developing drugs that target specific hormone receptors, like the use of small molecule agonists and antagonists to regulate thyroid hormone receptors.
  • Metabolism Regulation: Endocrinology research often focuses on metabolism and how hormones like insulin regulate it. Small molecules are employed to understand and develop drugs targeting enzymes involved in metabolism, such as glucagon-like peptide-1 (GLP-1) agonists for diabetes treatment.
  • Steroid Hormone Production: Small molecules may be utilized to influence the production of steroid hormones in the adrenal glands or gonads. This is essential for conditions like Cushing's syndrome or polycystic ovary syndrome (PCOS).
  • Hormone Assays: In laboratory research, small molecules are used as tracers or markers in hormone assays. For instance, small molecule fluorophores can be attached to antibodies to detect hormone levels in blood samples.

Drug Development: Endocrinology research relies on small molecules as potential drug candidates. Researchers design and test small molecules for their effectiveness in modulating hormonal pathways, with the goal of developing new therapies for endocrine disorders.
In summary, small molecules are indispensable tools in Endocrinology Research, enabling scientists to better understand the endocrine system's intricacies and develop novel treatments for a wide range of hormonal disorders and conditions. Their versatility and specificity make them valuable assets in advancing our knowledge of endocrinology and improving patient care.

Endocrinology Disease Products

Diabetes Research

Endocrinology Research Products

Kisspeptin Receptor

Leptin Receptors

Melanocortin (MC) Receptors

Mineralocorticoid Receptors

Galanin Receptors

TRH Receptors

Ghrelin Receptors

Natriuretic Peptide Receptors

NPY Receptors

Motilin Receptor

PTH Receptor

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Product Citation
  1. A10076
    Andarine (GTX-007)

    Androgen Receptor agonist

    Andarine (GTX-007) is an investigational selective androgen receptor modulator (SARM).
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  2. A10130
    Betamethasone dipropionate

    Glucocorticoid Receptor Agonist

    Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
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  3. A10439
    GSK1292263

    GPR119 agonist

    GSK-1292263 is a novel GPR119 agonist.
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  4. A10451
    Hexestrol

    Estrogen/progestogen Receptor agonist

    Hexestrol is a carcinogenic synthetic estrogen that inhibits microtubule polymerization and the formation of ribbon structures. It is an inhibitor of lipid peroxidation.
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  5. A10495
    Kaempferol

    ERRα and ERRγ inverse agonist

    Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.
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  6. A10550
    LY500307

    ERβ agonist

    LY500307 is a potent, selective estrogen receptor beta agonist with an EC50 of 0.66 nM.
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  7. A10582
    Methylprednisolone

    synthetic glucocorticoid receptor agonist

    Methylprednisolone is an apoptosis inducer and was also found to inhibit human small cell lung cancer cell growth in vitro.
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  8. A10752
    Prednisone (Adasone)

    Glucocorticoid Receptor agonist

    Prednisone reduces mucosal TNF-a production, intestinal permeability and levels of NF-kB expression.
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  9. A11431
    Glucocorticoid receptor agonist

    Glucocorticoid receptor agonist

    Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.
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  10. A11625
    Medroxyprogesterone Acetate

    progesterone receptor agonist

    Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
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  11. A11818
    Avobenzone

    estrogen agonist

    Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
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  12. A12311
    MK-6913

    Estrogen receptor β agonist

    Tetrahydrofluoroene 52 is a potent and selective estrogen receptor β agonist.
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  13. A12376
    SR 144528

    CB2 inverse agonist

    SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.
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  14. A12634
    MBX-2982

    GPR119 agonist

    MBX-2982 is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion.
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  15. A13193
    SR1001

    ROR agonist

    SR1001 is a selective ROR-alpha and ROR-gamma inverse agonist; suppresses TH17 cell differentiation and inhibits autoimmunity.
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  16. A13249
    AZD5423

    nonsteroidal glucocorticoid receptor agonist

    AZD5423 is a novel nonsteroidal glucocorticoid receptor agonist.
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  17. A13329
    Propyl pyrazole triol

    ERα agonist

    Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist.
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  18. A13359
    Diphenyleneiodonium chloride

    GPR3 agonist/NOS/ NADPH oxidases inhibitor

    Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells.
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  19. A13536
    AEZS-108

    GnRH-1 agonist

    AEZS-108 is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity.
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  20. A13568
    SR-2211

    RORr agonist

    SR-2211 selectively binds RORr(Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORr activity (IC50 = 320 nM).
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  21. A13716
    AR-231453

    GPR119 agonist

    AR-231453 is a potent and selective small molecule agonis of GPR119 that enhances glucose dependent insulin secretion and glucagon like peptide-1 (GLP-1) release.
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  22. A14342
    APD668

    GPR119 agonist

    APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.
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  23. A15071
    DY131

    ERRβ and ERRγ agonist

    DY131(GSK 9089) is a novel selective agonist of ERRα and ERRβ.
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  24. A15143
    Leuprolide Acetate

    GnRH agonist

    Leuprolide acetate is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors.
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  25. A15184
    Nestoron

    progesterone receptor agonist

    Nestoron is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive; a high-affinity agonist of the progesterone receptor.
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  26. A15241
    Sobetirome

    TRβ agonist

    Sobetirome is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively to TRβ-1 with EC50 of 0.16 μM.
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  27. A15245
    SR1078

    ROR agonist

    SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ; increases transcription of RORα target genes; thought to increase p53 stability.
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  28. A15246
    SR3335

    RORα agonist

    SR3335 is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays.
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  29. A15256
    Tanaproget

    Progesterone receptor agonist

    Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.
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  30. A15449
    JNJ 63533054

    GPR139 agonist

    JNJ 63533054 is a potent and selective GPR139 agonist with EC50 value of 16nm.
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  31. A15452
    APD597 (JNJ-38431055)

    GPR119 agonist

    APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
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  32. A15507
    6-OAU

    GPR84 agonist

    6-OAU is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.
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  33. A15959
    Goserelin Acetate

    GnRH agonist

    Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity.
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  34. A15997
    Triptorelin Acetate

    GnRH agonist

    Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts.
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  35. A16125
    SR-12813

    PXR agonist

    SR-12813 is a pregnane X receptor (PXR) agonist.
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  36. A16364
    TC-G-1008

    GPR39 agonist

    TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).
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  37. A16494
    Dexamethasone acetate

    glucocorticoid receptor agonist

    Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist.
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  38. A16863
    Cintirorgon (LYC-55716)

    RORγ agonist

    LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist.
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  39. A16956
    GSK4716

    ERRβ & ERRγ Agonist

    GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ
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  40. A16978
    Methylprednisolone hemisuccinate

    synthetic glucocorticoid receptor agonist

    Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
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  41. A16986
    (R)-Equol

    Estrogen receptor agonist

    (R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
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  42. A17002
    FAA1 agonist-1

    FAA1 agonist

    FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54.
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  43. A17080
    Dexamethasone Phosphate disodium

    glucocorticoid receptor agonist

    Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.
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  44. A17254
    Beclometasone dipropionate

    glucocorticoid agonist

    Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone.
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  45. A17574
    Canrenone

    Na/K ATPase partial agonist

    Canrenone is a metabolite of spironolactone, Na/K ATPase partial agonist and aldosterone and androgen receptor antagonist used as a diuretic.
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  46. A17986
    Leuprorelin Acetate

    GnRH/LHRH receptor agonist

    Leuprorelin is a Gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, LHRH) receptor agonist. Suppresses estradiol, LH and FSH serum levels and represses the growth of experimental rat endometriosis.
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  47. A17992
    Nafarelin Acetate

    GnRH agonist

    Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH.
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  48. A18177
    Beclometasone

    glucocorticoid receptor agonist

    Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma.
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  49. A18236
    Buserelin Acetate

    gonadotropin-releasing hormone agonist

    Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).
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  50. A18250
    Taltirelin

    TRH-R agonist

    Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).
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